Pyridinone derivatives: specific human immunodeficiency virus type 1 reverse transcriptase inhibitors with antiviral activity.
…, WA Schleif, KF Freund, SL Gaul… - Proceedings of the …, 1991 - National Acad Sciences
Derivatives of pyridinones were found to inhibit human immunodeficiency virus type 1 (HIV-1)
reverse transcriptase (RT) activity and prevent the spread of HIV-1 infection in cell culture …
reverse transcriptase (RT) activity and prevent the spread of HIV-1 infection in cell culture …
Transglutaminase inhibition by 2-[(2-oxopropyl) thio] imidazolium derivatives: mechanism of factor XIIIa inactivation
KF Freund, KP Doshi, SL Gaul, DA Claremon… - Biochemistry, 1994 - ACS Publications
Revised Manuscript Received May 16, 19948 abstract: The physiologic role of several
transglutaminases could be more precisely defined with the development of specific inhibitors for …
transglutaminases could be more precisely defined with the development of specific inhibitors for …
Preclinical pharmacology and pharmacokinetics of CERC‐301, a GluN2B‐selective N‐methyl‐D‐aspartate receptor antagonist
…, JA McCauley, RA Bednar, SL Gaul… - Pharmacology …, 2015 - Wiley Online Library
The preclinical pharmacodynamic and pharmacokinetic properties of 4‐methylbenzyl (3S,
4R)‐3‐fluoro‐4‐[(Pyrimidin‐2‐ylamino) methyl] piperidine‐1‐carboxylate ( CERC ‐301), an …
4R)‐3‐fluoro‐4‐[(Pyrimidin‐2‐ylamino) methyl] piperidine‐1‐carboxylate ( CERC ‐301), an …
Non-peptide GPIIb/IIIa inhibitors. 20. Centrally constrained thienothiophene α-sulfonamides are potent, long acting in vivo inhibitors of platelet aggregation
…, B Bednar, JD Prugh, RA Bednar, SL Gaul… - Journal of medicinal …, 1999 - ACS Publications
The synthesis and pharmacology of 4, a potent thienothiophene non-peptide fibrinogen
receptor antagonist, are reported. Compound 4 inhibited the aggregation of human gel-filtered …
receptor antagonist, are reported. Compound 4 inhibited the aggregation of human gel-filtered …
Identification and Characterization of 4-Methylbenzyl 4-[(Pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an Orally Bioavailable, Brain Penetrant NR2B Selective N-Methyl …
…, M Cunningham, AG DiLella, SL Gaul… - Journal of medicinal …, 2007 - ACS Publications
The discovery of a novel series of NR2B subtype selective N-methyl-d-aspartate (NMDA)
antagonists is reported. Initial optimization of a high-throughput screening lead afforded an …
antagonists is reported. Initial optimization of a high-throughput screening lead afforded an …
NR2B-Selective N-Methyl-d-aspartate Antagonists: Synthesis and Evaluation of 5-Substituted Benzimidazoles
…, RA Bednar, SD Mosser, SL Gaul… - Journal of medicinal …, 2004 - ACS Publications
Two classes of 5-substituted benzimidazoles were identified as potent antagonists of the
NR2B subtype of the N-methyl-d-aspartate (NMDA) receptor. Selected compounds show very …
NR2B subtype of the N-methyl-d-aspartate (NMDA) receptor. Selected compounds show very …
Orally efficacious NR2B-selective NMDA receptor antagonists
…, RA Bednar, SD Mosser, SL Gaul… - Bioorganic & Medicinal …, 2003 - Elsevier
… Author links open overlay panel Christopher F Claiborne a , John A McCauley a , Brian E
Libby a , Neil R Curtis b , Helen J Diggle b , Janusz J Kulagowski b , Stuart R Michelson a …
Libby a , Neil R Curtis b , Helen J Diggle b , Janusz J Kulagowski b , Stuart R Michelson a …
Non-peptide glycoprotein IIb/IIIa inhibitors. 17. Design and synthesis of orally active, long-acting non-peptide fibrinogen receptor antagonists
…, RJ Gould, RJ Lynch, JJ Lynch, SL Gaul… - Journal of medicinal …, 1997 - ACS Publications
The synthesis and pharmacological evaluation of 5 (L-738,167), a potent, selective non-peptide
fibrinogen receptor antagonist is reported. Compound 5 inhibited the aggregation of …
fibrinogen receptor antagonist is reported. Compound 5 inhibited the aggregation of …
Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1)
…, C Condra, J Karczewski, RA Bednar, SL Gaul… - Bioorganic & medicinal …, 2002 - Elsevier
The synthesis and biological evaluation of a series of nonpeptidic small molecule antagonists
of the human platelet thrombin receptor (PAR-1) are described. Optimization of the 5-…
of the human platelet thrombin receptor (PAR-1) are described. Optimization of the 5-…
Nonpeptide GPIIb/IIIa inhibitors. 10. Centrally constrained alpha-sulfonamides are potent inhibitors of platelet aggregation
…, B Bednar, RA Bednar, JJ Cook, SL Gaul… - Bioorganic & Medicinal …, 1996 - Elsevier
Potency enhancing features of two series of fibrinogen receptor antagonists were combined
to give analogs with improved potency and oral activity. Antagonists containing either alkyl …
to give analogs with improved potency and oral activity. Antagonists containing either alkyl …